Leupeptin hemisulfate

SKU: orb1300655

Description

Leupeptin hemisulfate is a cell-permeable, reversible, and competitive protease inhibitor active against Cathepsins B, H, and L. It is used in vitro and in vivo to study lysosomal function, protein degradation, and inflammatory processes in research areas like cancer and neurodegeneration.

Research Area

Cell Biology

Key Properties

• CAS Number: 103476-89-7
• MW: 475.6
• Purity: >95%; peptide content >85%
• Formula: C₂₀H₃₈N₆O₄ • 1/2H₂SO₄
• SMILES: OS(O)(=O)=O.CC(C)C[C@H](NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C=O.CC(C)C[C@H](NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C=O
• Target: Protease
• Solubility: Soluble in Water (up to 50 mg/ml). Also soluble in ethanol and methanol

Bioactivity

• Target IC50:
  Huh7 cells (SARS-CoV-2):39.29 µM (EC50)|SARS-CoV-2 (Vero cells):42.34 µM (EC50)|Human coronavirus strain 229E:0.4 µg/mL
• In Vivo:
  METHODS: To determine macrophage autophagic flux, Leupeptin hemisulfate (9-40 mg/kg in 0.5 mL PBS) was administered to C57BL/6NCrl mice by single intraperitoneal injection. RESULTS: Leupeptin hemisulfate treatment resulted in the highest accumulation of LC3b in the liver and the lowest in the spleen. LC3a, ATG8/LC3b homologs, and the LC3b-interacting protein p62 were degraded with kinetics similar to those of LC3b. METHODS: To examine whether cold activates autophagic flux, Leupeptin hemisulfate (40 mg/kg) was administered intraperitoneally to C57B6 mice in a single injection, and then the mice were cold-exposed at 4 ℃ for 1 h. The mice were then exposed to cold for 1 h. RESULTS: LC3-II flux in brown fat was increased >2-fold in cold-exposed mice.
• In Vitro:
  METHODS: SARS-CoV-2 infected Vero cells were treated with Leupeptin hemisulfate (0.06-200 µM) for 72 h, and the viral RNA level was detected by RT-PCR. RESULTS: Leupeptin hemisulfate inhibited SARS-CoV-2 RNA levels in Vero cells with an EC50 value of 42.34 µM. METHODS: SARS-CoV-2 pseudovirus-infected Huh7 cells were treated with Leupeptin hemisulfate (0.1-100 µM) for 24 h. Pseudovirus infection was detected by luciferase activity assay. RESULTS: Leupeptin hemisulfate inhibited pseudovirus infection in Vero cells with an EC50 value of 39.29 µM.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ac-Leu-Leu-Arg-CHO

Compound Identifiers

PubChem CID

2733491